Biginelli reaction is the most classical and frequently employed method for facile and diverse synthesis of 3,4-
dihydropyrimidinones and thiones (DHPMs)-a class of privileged heterocyclic scaffolds possessing meritorious biological and pharmacological
functions. Owing to the presence of a chiral centre in DHPMs and the discovered distinction in biological activity of DHPMs
isomers, accessing chiral DHPMs of optical purity constitutes a core issue of particular importance in the research of Biginelli reaction.
Following the rapid progress of modern organic synthesis, catalytic asymmetric Biginelli reaction has gradually evolved as the mainstream
method instead of early kinetic resolution for acquiring enantiomerically enriched. In the present paper, the advances in catalytic
asymmetric Biginelli reaction, including advances in metal catalysis as well as organocatalysis, are comprehensively reviewed.
Keywords: Asymmetric, Biginelli reaction, catalytic, DHPMs, enantioselective.
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